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WO2011049332A3 - Composés thiéno[3,2-d]pyrimidines substitués dans les positions 2 et 7 en tant qu'inhibiteurs de protéine kinase - Google Patents

Composés thiéno[3,2-d]pyrimidines substitués dans les positions 2 et 7 en tant qu'inhibiteurs de protéine kinase Download PDF

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Publication number
WO2011049332A3
WO2011049332A3 PCT/KR2010/007093 KR2010007093W WO2011049332A3 WO 2011049332 A3 WO2011049332 A3 WO 2011049332A3 KR 2010007093 W KR2010007093 W KR 2010007093W WO 2011049332 A3 WO2011049332 A3 WO 2011049332A3
Authority
WO
WIPO (PCT)
Prior art keywords
substituted thieno
protein kinase
kinase inhibitors
pyrimidine compounds
diseases caused
Prior art date
Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
Ceased
Application number
PCT/KR2010/007093
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English (en)
Other versions
WO2011049332A2 (fr
Inventor
Tae Bo Sim
Hwan Geun Choi
Jung Mi Hah
Young Jin Ham
Eun Jin Jun
Jung Hun Lee
Hwan Kim
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Korea Institute of Science and Technology KIST
Original Assignee
Korea Institute of Science and Technology KIST
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by Korea Institute of Science and Technology KIST filed Critical Korea Institute of Science and Technology KIST
Priority to EP10825157.0A priority Critical patent/EP2491043B1/fr
Priority to US13/503,125 priority patent/US8586580B2/en
Priority to JP2012535115A priority patent/JP5563662B2/ja
Priority to CN201080059034.8A priority patent/CN102712656B/zh
Publication of WO2011049332A2 publication Critical patent/WO2011049332A2/fr
Publication of WO2011049332A3 publication Critical patent/WO2011049332A3/fr
Anticipated expiration legal-status Critical
Ceased legal-status Critical Current

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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D495/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms
    • C07D495/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
    • C07D495/04—Ortho-condensed systems
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A61P35/02—Antineoplastic agents specific for leukemia
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D495/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms
    • C07D495/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D519/00—Heterocyclic compounds containing more than one system of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring system not provided for in groups C07D453/00 or C07D455/00

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Oncology (AREA)
  • Hematology (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Epidemiology (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)

Abstract

L'invention porte sur un composé thiéno[3,2-d]pyrimidine substitué dans les positions 2 et 7 ayant une activité d'inhibition des protéines kinases, sur un sel de qualité pharmaceutique et sur une composition pharmaceutique, comportant le composé en tant que principe actif, pour la prévention et le traitement de maladies provoquées par une croissance cellulaire anormale. Étant donné que le nouveau composé thiéno[3,2-d]pyrimidine substitué dans les positions 2 et 7 présente une activité d'inhibition supérieure à l'encontre de diverses protéines kinases mises en jeu dans la transduction du signal de facteur de croissance, ledit composé est utile en tant qu'agent de prévention ou de traitement de maladies provoquées par une croissance cellulaire anormale.
PCT/KR2010/007093 2009-10-22 2010-10-15 Composés thiéno[3,2-d]pyrimidines substitués dans les positions 2 et 7 en tant qu'inhibiteurs de protéine kinase Ceased WO2011049332A2 (fr)

Priority Applications (4)

Application Number Priority Date Filing Date Title
EP10825157.0A EP2491043B1 (fr) 2009-10-22 2010-10-15 COMPOSÉS THIÉNO[3,2-D]PYRIMIDINES SUBSTITUÉS DANS LES POSITIONS 2 ET 7 EN TANT QU'INHIBITEURS DE PROTÉINE KINASE& xA;
US13/503,125 US8586580B2 (en) 2009-10-22 2010-10-15 2,7-substituted thieno[3,2-d] pyrimidine compounds as protein kinase inhibitors
JP2012535115A JP5563662B2 (ja) 2009-10-22 2010-10-15 蛋白質キナーゼ阻害活性を有する２，７−置換されたチエノ［３，２−ｄ］ピリミジン化合物
CN201080059034.8A CN102712656B (zh) 2009-10-22 2010-10-15 作为蛋白激酶抑制剂的2,7-取代的噻吩并[3,2-d]嘧啶化合物

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
KR10-2009-0100867 2009-10-22
KR1020090100867A KR101147550B1 (ko) 2009-10-22 2009-10-22 단백질 키나아제 저해활성을 가지는 2,7-치환된 티에노［3,2-ｄ］피리미딘 화합물

Publications (2)

Publication Number Publication Date
WO2011049332A2 WO2011049332A2 (fr) 2011-04-28
WO2011049332A3 true WO2011049332A3 (fr) 2011-10-13

Family

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Family Applications (1)

Application Number Title Priority Date Filing Date
PCT/KR2010/007093 Ceased WO2011049332A2 (fr) 2009-10-22 2010-10-15 Composés thiéno[3,2-d]pyrimidines substitués dans les positions 2 et 7 en tant qu'inhibiteurs de protéine kinase

Country Status (6)

Country Link
US (1) US8586580B2 (fr)
EP (1) EP2491043B1 (fr)
JP (1) JP5563662B2 (fr)
KR (1) KR101147550B1 (fr)
CN (1) CN102712656B (fr)
WO (1) WO2011049332A2 (fr)

Cited By (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US9744176B2 (en) 2012-04-03 2017-08-29 Sanofi Therapeutic uses of novel thienopyrimidine derivatives

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EP2918588B1 (fr) 2010-05-20 2017-05-03 Array Biopharma, Inc. Composés macrocycliques comme inhibiteurs de la kinase TRK
JP5937112B2 (ja) 2011-02-17 2016-06-22 カンサー・セラピューティクス・シーアールシー・プロプライエタリー・リミテッドＣａｎｃｅｒ Ｔｈｅｒａｐｅｕｔｉｃｓ Ｃｒｃ Ｐｔｙ Ｌｉｍｉｔｅｄ 選択的ｆａｋ阻害剤
ES2691673T3 (es) 2011-02-17 2018-11-28 Cancer Therapeutics Crc Pty Limited Inhibidores de Fak
WO2012154009A2 (fr) * 2011-05-12 2012-11-15 한국화학연구원 Dérivés de thiénopyrimidine, leurs sels pharmaceutiquement acceptables, procédé de préparation de dérivés de thiénopyrimidine, et composition pharmaceutique contenant des dérivés de thiénopyrimidine en tant que principes actifs dans la prévention ou le traitement de maladies liées au diabète
KR20130013199A (ko) * 2011-07-27 2013-02-06 한미약품 주식회사 신규 피리미딘 유도체 및 이를 활성성분으로 포함하는 약학 조성물
BR112014015720B1 (pt) 2011-12-30 2020-03-17 Hanmi Pharm. Co., Ltd. Derivados de tieno[3,2-d]pirimidina, composição farmacêutica e uso dos mesmos para a prevenção ou tratamento de uma doença causada por ativação anormal de uma proteína quinase
JP6109193B2 (ja) * 2012-01-10 2017-04-05 エフ・ホフマン−ラ・ロシュ・アクチェンゲゼルシャフト チエノピリミジン化合物
TWI585088B (zh) * 2012-06-04 2017-06-01 第一三共股份有限公司 作爲激酶抑制劑之咪唑并［１，２－ｂ］嗒衍生物
KR101704386B1 (ko) * 2013-06-28 2017-02-08 한국과학기술연구원 티에노[3,2-ｄ]피리미딘 유도체의 Ｔ315Ｉ-Ｂｃｒ-Ａｂｌ 점돌연변이종의 저해 활성
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KR20160005664A (ko) * 2014-07-07 2016-01-15 한국과학기술연구원 약물 부작용이 감소된 급성골수성백혈병 표적치료제
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CN106366093B (zh) * 2015-07-21 2020-08-18 广州再极医药科技有限公司 稠环嘧啶类化合物、中间体、其制备方法、组合物和应用
WO2017184844A1 (fr) * 2016-04-21 2017-10-26 Duke University Inhibiteurs de l'acide gras synthase
TWI704148B (zh) 2016-10-10 2020-09-11 美商亞雷生物製藥股份有限公司 作為ｒｅｔ激酶抑制劑之經取代吡唑并[1,5-a]吡啶化合物
JOP20190077A1 (ar) 2016-10-10 2019-04-09 Array Biopharma Inc مركبات بيرازولو [1، 5-a]بيريدين بها استبدال كمثبطات كيناز ret
KR101812266B1 (ko) 2016-11-25 2017-12-27 한국과학기술연구원 4-((2-아크릴아미도페닐)아미노)티에노[3,2-d]피리미딘-7-카복스아미드 유도체 및 그의 약학적 활용
AU2017369753A1 (en) * 2016-12-01 2019-07-18 Aptose Biosciences Inc. Fused pyrimidine compounds as BRD4 and JAK2 dual inhibitors and methods for use thereof
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CA3049136C (fr) 2017-01-18 2022-06-14 Array Biopharma Inc. Composes de pyrazolo[1,5-a]pyrazine substitues utilises en tant qu'inhibiteurs de la kinase ret
JOP20190213A1 (ar) 2017-03-16 2019-09-16 Array Biopharma Inc مركبات حلقية ضخمة كمثبطات لكيناز ros1
TWI791053B (zh) 2017-10-10 2023-02-01 美商亞雷生物製藥股份有限公司 6-(2-羥基-2-甲基丙氧基)-4-(6-(6-((6-甲氧基吡啶-3-基)甲基)-3,6-二氮雜雙環[3.1.1]庚-3-基)吡啶-3-基)吡唑并[1,5-a]吡啶-3-甲腈之結晶形式及其醫藥組合物
TWI812649B (zh) 2017-10-10 2023-08-21 美商絡速藥業公司 6-(2-羥基-2-甲基丙氧基)-4-(6-(6-((6-甲氧基吡啶-3-基)甲基)-3,6-二氮雜雙環[3.1.1]庚-3-基)吡啶-3-基)吡唑并[1,5-a]吡啶-3-甲腈之調配物
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WO2019143994A1 (fr) 2018-01-18 2019-07-25 Array Biopharma Inc. Composés de pyrazolyl[4,3-c]pyridine substitués utilisés en tant qu'inhibiteurs de la kinase ret
CA3087354C (fr) 2018-01-18 2023-01-03 Array Biopharma Inc. Composes de pyrrolo[2,3-d]pyrimidines substitues utilises en tant qu'inhibiteurs de la kinase ret
CA3087578C (fr) 2018-01-18 2023-08-08 Array Biopharma Inc. Composes de pyrazolo[3,4-d]pyrimidine substitues utilises en tant qu'inhibiteurs de la kinase ret
CN112996794A (zh) 2018-09-10 2021-06-18 阿雷生物药品公司 作为ret激酶抑制剂的稠合杂环化合物
WO2020231708A1 (fr) 2019-05-10 2020-11-19 The Regents Of The University Of California Procédés de prolongement de la durabilité de dispositifs électrochimiques à oxyde solide sur support métallique
WO2023169461A1 (fr) * 2022-03-08 2023-09-14 广州再极医药科技有限公司 Composé thiénopyrimidine, intermédiaire, procédé de préparation correspondant, composition et utilisation associées
WO2023246371A1 (fr) * 2022-06-24 2023-12-28 中国科学院基础医学与肿瘤研究所(筹) Composé à petites molécules ayant une structure pyrimidothiophène et son utilisation
CN116478168B (zh) * 2023-03-31 2024-11-29 杭州医学院 一种具有fak抑制活性的化合物、制备方法及其应用
CN118165003B (zh) * 2024-03-13 2024-10-18 江西科技师范大学 含噻喃并嘧啶类化合物及其应用

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Cited By (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US9744176B2 (en) 2012-04-03 2017-08-29 Sanofi Therapeutic uses of novel thienopyrimidine derivatives
US10220044B2 (en) 2012-04-03 2019-03-05 Sanofi Thienopyrimidine derivatives, processes for the preparation thereof and therapeutic uses thereof
US10500212B2 (en) 2012-04-03 2019-12-10 Sanofi Thienopyrimidine derivatives, processes for the preparation thereof and therapeutic uses thereof
US10736904B2 (en) 2012-04-03 2020-08-11 Sanofi Thienopyrimidine derivatives, processes for the preparation thereof and therapeutic uses thereof
US10980816B2 (en) 2012-04-03 2021-04-20 Sanofi Thienopyrimidine derivatives, processes for the preparation thereof and therapeutic uses thereof

Also Published As

Publication number Publication date
US20120277424A1 (en) 2012-11-01
CN102712656B (zh) 2016-01-20
KR101147550B1 (ko) 2012-05-17
KR20110044053A (ko) 2011-04-28
EP2491043A2 (fr) 2012-08-29
EP2491043B1 (fr) 2014-07-16
EP2491043A4 (fr) 2013-05-22
JP2013508354A (ja) 2013-03-07
WO2011049332A2 (fr) 2011-04-28
CN102712656A (zh) 2012-10-03
US8586580B2 (en) 2013-11-19
JP5563662B2 (ja) 2014-07-30

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